Louse repellent compositions

Abstract: The use of a compound of general formula I in the manufacture of a medicament having pediculicidal or louse repellent properties A is -CH₂OR, -CHO, -CO₂R¹ wherein R is H, C₁ to C₅ alkyl or and R¹ is H or C₁ to C₃ alkyl

Description: The invention relates to louse repellent compositions. US 2 400 006 describes the use of ortho and para alkoxyphenylalkyl alcohols of specified structure as repellent for Trombiculidae, Aedes aegypti, Aedes taeniorhynchus and Anopheles quadrimaculatus. We have surprisingly found that a range of methoxy aromatic compounds have louse repellent and pediculicidal properties. According to the invention there is provided the use of a compound of general formula I in the manufacture of a medicament having pediculicidal or louse repellent properties. A is -CH 2 OR, -CHO, -CC 2 R 1 wherein R is H, C 1 to C 5 alkyl or and R 1 is H or C 1 to C 3 alkyl The para isomer is often somewhat preferred on cost grounds but ortho and meta isomers are both usable. Some of the compounds such as p-anisaldehyde have agreeable odours and may be preferred. Preferred compounds of the invention include 4-methoxybenzaldehyde (II), 4-methoxybenzoic acid (III), 4-methoxybenzyl alcohol (IV) and p-anisyl p-anisicate (V) At least some of the compounds are readily available commercially. Those skilled in the art will readily be able to obtain others. The active ingredient is conveniently applied directly to the hair. Those skilled will readily be able to devise vehicles for doing this. Convenient forms include lotions gels and mousses which may be prepared in a manner familiar to those skilled in the art. Preferably the compounds are presented in alcoholic solution. The alcohol may be ethanol, propanol especially isopropanol, other alcohols or mixtures thereof. Preferably aqueous alcohol is used to reduce the possibility of skin irritation. The efficiency of the composition may be enhanced by ensuring that it has a tendency to coat the hair. This can be achieved by incorporating spreading film formers such as silicones, soluble lanolin or soluble polymers such as PVP optionally copolymerised with vinyl acetate. Many of the compounds of the invention are solid at room temperature and may have a tendency to crystallise from alcohol solution at low temperature eg about 0°C. The crystals may block the dispenser. This problem can be substantially reduced by incorporating an emulsifier. Preferably two emulsifiers are employed. A, the or each emulsifier may be an nonionic emulsifier such as alkoxylated fatty alcohol or fatty acid. The emulsifier keeps the active ingredient in solution and deters crystallisation. Where two emulsifiers are used the solubilisation appears to be increased synergistically. Where emulsifier is present the active ingredient tends to form a film rather than to crystallise rapidly in use. High alcohol concentrations are preferably avoided to reduce the possibility of irritation. Furthermore the comparatively high water content makes the composition pleasant to use. Preferred concentrations of active are from about 0.5 to 1 wt% more preferably 1 to 3 wt%. The compositions may also preferably contain phenoxyethanol as an antimicrobial preservative. Examples of the invention will now be described by way of illustration. Example 1 An aqueous alcoholic mousse was prepared by heating to 60°C all the following components other than the propellant. The warm mixture was transferred to aerosol containers and charged with propellant in the usual way. wt% p-Anisaldehyde 2-10 Ethanol 50 Water qs Propylene glycol 5 Polawax A31 5 Propellant Polawax A31 is an ethoxylated cetostearyl alcohol oil in water emulsifying wax. It is designated Ceteareth-20 by the CTFA. Example 2 An aqueous alcoholic lotion was prepared by mixing the following components: wt% p-Anisaldehyde 2-10 Eumulgin RO40 1-10 Eumulgin L 5-30 Water qs Eumulgin RO40 is an ethoxylated castor oil and Eumulgin L is a 2-hydroxy fatty acid alkoxylate. Both are available from Henkel AG. Example 3 An aqueous alcoholic lotion was prepared by mixing the following ingredients: wt% p-Anisaldehyde 2-10 Dow Corning 190 0.5-2.0 Ethanol 15-40 Isopropanol 5-30% Water qs Dow Corning 190 is modified silicone fluid. Example 4 An aqueous alcoholic lotion was prepared in a similar manner to the lotion of Example 3. However the Dow Corning 190 was replaced by 1-3 wt% of the soluble lanolin Lanexol AWS. Example 5 An aqueous alcoholic lotion was prepared in the same way as the lotion of Example 3. However the Dow Corning 190 was replaced by 1-3 wt% of a soluble polymer of the Kollidon series which are polyvinylpyrollidones which are copolymerised in some cases with vinyl acetate.

Claims: The use of a compound of general formula I in the manufacture of a medicament having pediculicidal or louse repellent properties A is =CH 2 OR, -CHO, -CO 2 R 1 wherein R is H, C 1 to C 5 alkyl or and R 1 is H or C 1 to C 3 alkyl The use as claimed in claim 1 wherein the compound of general formula I is 4-methoxybenzaldehyde, 4-methoxybenzoic acid, 4-methoxybenzyl alcohol or p-anisyl p-anisicate. The use as claimed in claim 2 wherein the compound of general formula I is 4-methoxybenzaldehyde. A pediculicidal or louse repellent composition comprising: i) at least 0.5 wt. % of a compound of formula I wherein R is C 1 to C 5 alkyl ii) aqueous alcohol, and iii) an emulsifier, or iv) a spreading film former. A composition as claimed in claim 4 wherein the emulsifier comprises ethoxylated castor oil fatty acids. A composition as claimed in claim 4 or 5 wherein component iv) is a silicone, lanolin or polyvinylpyrrolidone. A composition as claimed in any one of claims 4 to 6 wherein the compound of formula I is 4-methoxybenzaldehyde.

Inventors: IRWIN RICHARD NEIL, IRWIN, RICHARD NEIL
Applicants: UNICLIFFE LTD, UNICLIFFE LIMITED
Application year: 1994
Main classification: A01N35
IPC codes: A01N35, A61K31, A01N31, A01N37